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A2B Adenosine Receptor and Cancer

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, USA
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Int. J. Mol. Sci. 2019, 20(20), 5139; https://doi.org/10.3390/ijms20205139
Received: 25 September 2019 / Revised: 11 October 2019 / Accepted: 12 October 2019 / Published: 17 October 2019
(This article belongs to the Special Issue G Protein-Coupled Adenosine Receptors: Molecular Aspects and Beyond)
There are four subtypes of adenosine receptors (ARs), named A1, A2A, A2B and A3, all of which are G protein-coupled receptors (GPCRs). Locally produced adenosine is a suppressant in anti-tumor immune surveillance. The A2BAR, coupled to both Gαs and Gαi G proteins, is one of the several GPCRs that are expressed in a significantly higher level in certain cancer tissues, in comparison to adjacent normal tissues. There is growing evidence that the A2BAR plays an important role in tumor cell proliferation, angiogenesis, metastasis, and immune suppression. Thus, A2BAR antagonists are novel, potentially attractive anticancer agents. Several antagonists targeting A2BAR are currently in clinical trials for various types of cancers. In this review, we first describe the signaling, agonists, and antagonists of the A2BAR. We further discuss the role of the A2BAR in the progression of various cancers, and the rationale of using A2BAR antagonists in cancer therapy. View Full-Text
Keywords: adenosine receptor; immune system; cancer therapy; tumor microenvironment; cell proliferation; metastasis adenosine receptor; immune system; cancer therapy; tumor microenvironment; cell proliferation; metastasis
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Gao, Z.-G.; Jacobson, K.A. A2B Adenosine Receptor and Cancer. Int. J. Mol. Sci. 2019, 20, 5139.

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